近日，FDA批准新药Zypitamag（pitavastatin）用于原发性高脂血症或混合性血脂异常的患者，作为饮食的辅助疗法，以降低总胆固醇（TC），低密度脂蛋白胆固醇（LDL-C），载脂蛋白 B（Apo B），甘油三酯（TG），并增加高密度脂蛋白胆固醇（HDL-C）。
批准日期：2017年7月14日 公司：Medicure International Inc
ZYPITAMAG（匹伐他汀[pitavastatin]）片剂，用于口服
美国最初批准：2009年
作用机制
匹伐他汀以与底物竞争的方式竞争性抑制HMG-CoA还原酶，HMG-CoA还原酶是涉及胆固醇生物合成的速率决定酶，因此它抑制肝脏中的胆固醇合成。结果，LDL-受体的表达随后从血液到肝脏摄取LDL加速，然后血浆TC降低。 此外，肝脏中胆固醇合成的持续抑制降低了极低密度脂蛋白的水平。
适应症和用法
ZYPITAMAG是一种HMG-CoA还原酶抑制剂，适用于：
原发性高脂血症或混合性血脂异常的患者作为饮食的辅助治疗，以降低升高的总胆固醇（TC），低密度脂蛋白胆固醇（LDL-C），载脂蛋白B（Apo B），甘油三酯（TG），并增加高血脂密度脂蛋白胆固醇（HDL-C）。
使用限制：
每日一次大于4毫克的剂量与在上市前临床研究中严重肌病的风险增加相关。每日一次给药不要超过4毫克。
ZYPITAMAG对心血管疾病发病率和死亡率的影响尚未确定。
ZYPITAMAG尚未在Fredrickson I型，III型和V型血脂异常中进行过研究。
剂量和给药
可以在一天中的任何时间带或不带食物。
剂量范围：每日1毫克至4毫克。
原发性高脂血症和混合性血脂异常：起始剂量2mg。当LDL-C的降低不足时，剂量可以增加至每天最多4mg。
中度和重度肾功能损害和血液透析终末期肾病：每日一次1毫克的起始剂量，每日一次最大剂量2毫克。
剂量形式和强度
片剂：1mg，2mg和4mg。
禁忌症
已知对产品成分的超敏感性。
活动性肝病，可能包括肝转氨酶水平不明原因持续升高。
怀孕。
哺乳期。
与环孢菌素共同给药。
警告和注意事项
骨骼肌效应（例如，肌病和横纹肌溶解症）：风险以剂量依赖性方式增加，伴有高龄（≥65），肾功能损害和治疗不足甲状腺功能减退。建议患者及时报告不明原因和/或持续性肌肉疼痛，压痛或虚弱，并停止使用ZYPITAMAG。
肝酶异常：肝转氨酶持续升高。在开始治疗之前检查肝酶测试，之后进行临床指示。
不良反应
最常见的不良反应（在至少一种上市剂量中≥2％）是肌痛，背痛，腹泻，便秘和四肢疼痛。
药物相互作用
红霉素：组合增加匹伐他汀暴露。每日一次限制ZYPITAMAG至1毫克。
利福平：联合用药可增加匹伐他汀的摄入量。每日一次限制ZYPITAMAG至2毫克。
伴随降脂疗法：使用贝特类或脂质修饰剂量（≥1克/天）的烟酸可增加不良骨骼肌效应的风险。使用ZYPITAMAG处方时应谨慎使用。
用于特定人群
女性和生殖潜力的男性：建议女性在治疗期间使用有效的避孕措施。
儿科用途：尚未确定安全性和有效性。
包装提供/存储和处理
ZYPITAMAG（匹伐他汀）片剂，按如下方式提供：
ZYPITAMAG 1 MG TAB 90 PITAVASTATIN MAGNESIUM MEDICURE PHARMA 25208020009
ZYPITAMAG 2 MG TAB 90 PITAVASTATIN MAGNESIUM MEDICURE PHARMA 25208020109
ZYPITAMAG 4 MG TAB 90 PITAVASTATIN MAGNESIUM MEDICURE PHARMA 25208020209
存储
储存温度为20°C至25°C（68°F至77°F）[参见USP Controlled Room Temperature]。防潮和防光。
完整说明资料附件：
https://www.zypitamag.com/docs/prescribing_information.pdf?v=20190619034913
ZYPITAMAG(pitavastatin)tablets, for oral use
IMPORTANT SAFETY INFORMATION FOR ZYPITAMAG™ (pitavastatin)
INDICATIONS & USAGE
Drug therapy should be one component of multiple-risk-factor intervention in individuals who require modifications of their lipid profile. Lipid-altering agents should be used in addition to a diet restricted in saturated fat and cholesterol only when the response to diet and other nonpharmacological measures has been inadequate.
Primary Hyperlipidemia and Mixed Dyslipidemia: Zypitamag™ is indicated as an adjunctive therapy to diet to reduce elevated total cholesterol (TC), low-density lipoprotein cholesterol (LDL-C), apolipoprotein B (Apo B), triglycerides (TG), and to increase high-density lipoprotein cholesterol (HDL-C) in adult patients with primary hyperlipidemia or mixed dyslipidemia.
Limitations of Use: Doses of Zypitamag™ greater than 4 mg once daily were associated with an increased risk for severe myopathy in premarketing clinical studies. Do not exceed 4 mg once daily dosing of Zypitamag™. The effect of Zypitamag™ on cardiovascular morbidity and mortality has not been determined. Zypitamag™ has not been studied in Fredrickson Type I, III, and V dyslipidemias.
CONTRAINDICATIONS
Zypitamag™ is contraindicated in patients with a known hypersensitivity to product components, in patients with active liver disease (which may include unexplained persistent elevations in hepatic transaminase levels), in women who are pregnant or may become pregnant, in nursing mothers or in coadministration with cyclosporine.
WARNINGS & PRECAUTIONS
Skeletal Muscle Effects: Cases of myopathy and rhabdomyolysis with acute renal failure secondary to myoglobinuria have been reported with HMG-CoA reductase inhibitors, including pitavastatin.
These risks can occur at any dose level, but increase in a dose-dependent manner, with advanced age (≥ 65 years), renal impairment, and inadequately treated hypothyroidism; administer with caution in these patients, or when used concomitantly with fibrates or lipid-modifying doses of niacin, or colchicine. Avoid concomitant administration with gemfibrozil.
Advise patients to promptly report unexplained and/or persistent muscle pain, tenderness, or weakness, particularly if accompanied by malaise or fever; discontinue Zypitamag™.
If muscle signs and symptoms persist after discontinuation, this may be a sign of immune-mediated necrotizing myopathy (IMNM), an autoimmune myopathy associated with statin use, requiring immediate medical attention. IMNM is characterized by proximal muscle weakness and elevated serum creatine kinase, which persist despite discontinuation of statin treatment; muscle biopsy showing necrotizing myopathy without significant inflammation; improvement with immunosuppressive agents.
Zypitamag™ should be discontinued if markedly elevated creatine kinase levels occur or myopathy is diagnosed or suspected.
Zypitamag™ should also be temporarily withheld in any patient with an acute, serious condition suggestive of myopathy or predisposing to the development of renal failure secondary to rhabdomyolysis (e.g., sepsis, hypotension, dehydration, major surgery, trauma, severe metabolic, endocrine, and electrolyte disorders, or uncontrolled seizures).
Liver Enzyme Abnormalities:
Persistent elevation in hepatic transaminases can occur. Check liver enzymes before initiating therapy and if signs or symptoms of liver injury occur; advise patients to report fatigue, anorexia, right upper abdominal discomfort, dark urine or jaundice.
Fatal and non-fatal hepatic failure can occur. Interrupt Zypitamag™ if serious liver injury with clinical symptoms and/or hyperbilirubinemia or jaundice occurs. If an alternate etiology is not found do not restart Zypitamag™.
Use Zypitamag™ with caution in patients who consume substantial quantities of alcohol and/or have a history of chronic liver disease. Do not use Zypitamag™ if patient has active liver disease, which may include unexplained persistent transaminase elevations.
Endocrine Function:
Increases in HbA1c and fasting serum glucose levels have been reported.
COMMON ADVERSE REACTIONS
Myalgia, back pain, diarrhea, constipation and pain in extremity (rate ≥ 2% in at least one marketed dose). This is not a complete list of all reported adverse events.